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Literature summary for 1.8.1.9 extracted from

  • Vergara, E.; Casini, A.; Sorrentino, F.; Zava, O.; Cerrada, E.; Rigobello, M.P.; Bindoli, A.; Laguna, M.; Dyson, P.J.
    Anticancer therapeutics that target selenoenzymes: synthesis, characterization, in vitro cytotoxicity, and thioredoxin reductase inhibition of a series of gold(I) complexes containing hydrophilic phosphine ligands (2010), ChemMedChem, 5, 96-102.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4-methylpyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
-
Homo sapiens
(4-methylpyrimidine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
-
Homo sapiens
(pyridine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
-
Homo sapiens
(pyridine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
-
Homo sapiens
(pyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
-
Homo sapiens
auranofin
-
Homo sapiens
cisplatin
-
Homo sapiens
trisodium (4,5-dihydro-1,3-thiazole-2-thiolato-kappaS2)[3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)]aurate(3-)
-
Homo sapiens
trisodium [3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)](pyrimidine-2-thiolato-kappaS)aurate(3-)
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol isoform TrxR2 Homo sapiens 5829
-
mitochondrion isoform TrxR2 Homo sapiens 5739
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-2780 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
Homo sapiens 2-nitro-5-thiobenzoate + NADP+
-
?

Synonyms

Synonyms Comment Organism
thioredoxin reductase
-
Homo sapiens
TrxR1 isoform Homo sapiens
TrxR2 isoform Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD
-
Homo sapiens
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000062
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens trisodium [3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)](pyrimidine-2-thiolato-kappaS)aurate(3-)
0.00000074
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens auranofin
0.00000096
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (4-methylpyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000154
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyridine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
0.00000155
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (4-methylpyrimidine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
0.00000161
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyridine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000167
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens trisodium (4,5-dihydro-1,3-thiazole-2-thiolato-kappaS2)[3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)]aurate(3-)
0.00000192
-
isoform TrxR1, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000245
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens auranofin
0.00000406
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (4-methylpyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000412
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyridine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000586
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (4-methylpyrimidine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
0.0000062
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyridine-2-thiolato-kappaS)[1,1'-(1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane-3,7-diyl-kappaP)diethanone]gold
0.00000673
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens (pyrimidine-2-thiolato-kappaS)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
0.00000682
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens trisodium (4,5-dihydro-1,3-thiazole-2-thiolato-kappaS2)[3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)]aurate(3-)
0.00000695
-
isoform TrxR2, in 0.2 M Na/K phosphate buffer (pH 7.4), at 37°C Homo sapiens trisodium [3,3',3''-(phosphanetriyl-kappaP)tribenzenesulfonato(3-)](pyrimidine-2-thiolato-kappaS)aurate(3-)